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ES2236180T3 - ANTIALERGIC OPHTHALMIC COMPOSITIONS SUITABLE FOR USE WITH CONTACT LENSES. - Google Patents

ANTIALERGIC OPHTHALMIC COMPOSITIONS SUITABLE FOR USE WITH CONTACT LENSES.

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Publication number
ES2236180T3
ES2236180T3 ES01906672T ES01906672T ES2236180T3 ES 2236180 T3 ES2236180 T3 ES 2236180T3 ES 01906672 T ES01906672 T ES 01906672T ES 01906672 T ES01906672 T ES 01906672T ES 2236180 T3 ES2236180 T3 ES 2236180T3
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volume
weight
allergic
emedastine
olopatadine
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ES01906672T
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John M. Yanni
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Alcon Inc
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Alcon Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Compositions Of Macromolecular Compounds (AREA)

Abstract

Topically administrable anti-allergy compositions comprising olopatadine and a polymeric quaternary ammonium preservative are suitable for use by patients wearing contact lenses.

Description

Composiciones oftálmicas antialérgicas adecuadas para uso con lentes de contacto.Suitable anti-allergic ophthalmic compositions For use with contact lenses.

Antecedentes de la invenciónBackground of the invention

La presente invención se refiere generalmente a composiciones oftálmicas anti-alérgicas. En particular, la presente invención se refiere a composiciones tópicas anti-alérgicas que pueden aplicarse de forma segura a un paciente que lleva lentes de contacto.The present invention generally relates to anti-allergic ophthalmic compositions. In In particular, the present invention relates to compositions anti-allergic topics that can be applied safe for a patient wearing contact lenses.

Las formulaciones oftálmicas contienen generalmente uno o más compuestos activos junto con excipientes tales como tensioactivos, agentes reconfortantes, agentes complejantes, estabilizadores, sistemas tamponantes, agentes quelantes, agentes de viscosidad o polímeros gelificantes y antioxidantes. Las formulaciones oftálmicas que están pensadas para uso multi-dosis requieren un conservante. El cloruro de benzalconio ("BAC") es el conservante oftálmico más ampliamente usado.Ophthalmic formulations contain generally one or more active compounds together with excipients such as surfactants, comforting agents, agents complexing agents, stabilizers, buffer systems, agents chelators, viscosity agents or gelling polymers and antioxidants Ophthalmic formulations that are designed to Multi-dose use require a preservative. He benzalkonium chloride ("BAC") is the most ophthalmic preservative widely used

Los productos oftálmicos multi-dosis administrables tópicamente no son generalmente adecuados para usar con lentes de contacto porque el compuesto activo o el conservante puede enlazarse a o acumularse en las lentes de contacto, provocando irritación o efectos tóxicos.Ophthalmic products Topically administrable multi-doses are not generally suitable for use with contact lenses because the active compound or preservative can bind to or accumulate in contact lenses, causing irritation or effects Toxic

La olopatadina es un medicamento anti-alérgico conocido. Véase la Patente de EE.UU. núm. 5.641.805 (Yanni, et al.) PATANOL®, marca de solución oftálmica de hidrocloruro de olopatadina, se comercializa como una composición tópica anti-alérgica. La emedastina es un medicamento anti-histamínico conocido. EMADINE®, marca de solución de difumarato de emedastina, se comercializa como una composición tópica anti-alérgica. Como otros productos anti-alérgicos administrables tópicamente, estas composiciones se conservan con BAC. BAC es conocido por enlazarse a o acumularse en las lentes de contacto. Así, como otros productos farmacéuticos oftálmicos administrables tópicamente que contienen BAC, PATANOL®, marca de solución oftálmica de hidrocloruro de olopatadina y EMADINE®, marca de solución oftálmica de difumarato de emedastina, contienen en su información etiquetada, instrucciones de precaución para quitar las lentes de contacto antes del uso y esperar diez minutos después de administrar el producto antes de ponerse de nuevo las lentes. El régimen de dosificación para productos anti-alérgicos típicamente piden dos a cuatro aplicaciones al día, haciéndolos inconvenientes para tratar los síntomas oftálmicos de la alergia a los usuarios de lentes de contacto.Olopatadine is a known anti-allergic medication. See US Pat. no. 5,641,805 (Yanni, et al .) PATANOL®, brand of ophthalmic solution of olopatadine hydrochloride, is marketed as a topical anti-allergic composition. Emedastine is a known anti-histamine medication. EMADINE®, brand of emedastine dipumate solution, is marketed as a topical anti-allergic composition. Like other topically administrable anti-allergic products, these compositions are preserved with BAC. BAC is known to bind to or accumulate in contact lenses. Thus, like other topically administrable ophthalmic pharmaceutical products that contain BAC, PATANOL®, olopatadine hydrochloride ophthalmic solution brand and EMADINE®, emedastine difumate ophthalmic solution brand, they contain in their labeled information, precautionary instructions to remove the lenses contact before use and wait ten minutes after administering the product before putting the lenses back on. The dosage regimen for anti-allergic products typically requires two to four applications a day, making them inconvenient to treat ophthalmic symptoms of allergy to contact lens wearers.

El poliquaternium-1, que se usa bajo la marca registrada Polyquad®, es un conservante conocido por ser compatible con lentes de contacto. El poliquaternium-1 y otros compuestos poliméricos de amonio cuaternario se usan como desinfectantes y conservantes en el cuidado de lentes de contacto y soluciones de lágrima artificial. Véase, por ejemplo, las Patentes de EE.UU. núms. 5.037.647; 4.525.346 y 4.407.791. La marca de productos de cuidado de lentes de contacto comercializada normalmente como Opti-Free®, que incluye soluciones multi-uso y soluciones de limpieza, contiene poliquaternium-1 como un desinfectante y conservante.Polyquaternium-1, which is used under the trademark Polyquad®, it is a preservative known for Be compatible with contact lenses. He polyquaternium-1 and other polymeric compounds of Quaternary ammonium are used as disinfectants and preservatives in the contact lens care and artificial tear solutions. See, for example, US Pat. no. 5,037,647; 4,525,346 and 4,407,791. The brand of lens care products contact normally marketed as Opti-Free®, which includes solutions multi-use and cleaning solutions, contains polyquaternium-1 as a disinfectant and preservative

Además de en productos del cuidado de lentes de contacto, el poliquaternium-1 puede usarse además como un conservante en ciertos productos farmacológicos oftálmicos administrables tópicamente. La Patente de EE.UU. núm. 5.603.929 describe el uso de poliquaternium-1 en combinación con ácido bórico para conservar las composiciones oftálmicas administrables tópicamente de medicamentos ácidos, tales como medicamentos anti-inflamatorios no esteroidales. Aunque la patente `929 define compuestos farmacológicos oftálmicos adecuados para usar con el sistema de conservación de poliquaternium-1 y ácido bórico que incluyen sales, amidas, ésteres y promedicamentos aceptables oftálmicamente de los muchos tipos de medicamentos ácidos, no menciona los medicamentos anti-alérgicos o la olopatadina en particular. Véase Col. 3, líneas 12-30 de la patente `929.In addition to lens care products from contact, polyquaternium-1 can also be used as a preservative in certain ophthalmic pharmacological products Topically administrable. U.S. Pat. no. 5,603,929 describes the use of polyquaternium-1 in combination with boric acid to preserve ophthalmic compositions topically administrable of acidic medications, such as non-steroidal anti-inflammatory drugs. Although the `929 patent defines ophthalmic pharmacological compounds suitable for use with the preservation system of polyquaternium-1 and boric acid that include salts, ophthalmically acceptable amides, esters and averages of the Many types of acid medications, does not mention medications anti-allergic or olopatadine in particular. See Col. 3, lines 12-30 of the `929 patent.

El documento US-A 5.192.780 describe una composición oftálmica que contiene 1-(2-etoxietil)-2-(4-metil-1-homopiperazinil)-bencimidazol y cloruro de benzalconio. Este documento no describe problemas que pudieran ocurrir si una persona que lleva lentes de contacto tiene que usar una solución oftálmica.US-A 5,192,780 describes an ophthalmic composition that contains 1- (2-ethoxyethyl) -2- (4-methyl-1-homopiperazinyl) -benzimidazole and benzalkonium chloride. This document does not describe problems that could occur if a person wearing contact lenses has Than using an ophthalmic solution.

Compendio de la invenciónCompendium of the invention

Se ha descubierto ahora que las composiciones de olopatadina y emedastina o sus sales farmacéuticamente aceptables, que comprenden poliquaternium-1 como un conservante, son adecuadas para usar con lentes de contacto. La presente invención se refiere a composiciones multi-dosis, administrables tópicamente, de olopatadina y emedastina o sus sales farmacéuticamente aceptables, que contienen un compuesto polimérico de amonio cuaternario, tal como poliquaternium-1, como un conservante. Las composiciones de la presente invención no contienen BAC.It has now been discovered that the compositions of olopatadine and emedastine or their pharmaceutically acceptable salts, comprising polyquaternium-1 as a preservative, are suitable for use with contact lenses. The present invention relates to compositions multi-dose, topically administrable, of olopatadine and emedastine or their pharmaceutically acceptable salts, containing a polymeric quaternary ammonium compound, such as polyquaternium-1, as a preservative. The Compositions of the present invention do not contain BAC.

La presente invención se refiere además al uso de una cantidad anti-alérgica eficaz de un medicamento seleccionado del grupo que consiste en olopatadina y emedastina y sus sales farmacéuticamente aceptables, en combinación con un compuesto polimérico de amonio cuaternario como un conservante, para la preparación de una composición administrable tópicamente para tratar o controlar las alergias oculares en pacientes que llevan lentes de contacto y en la que la composición puede aplicarse sin quitarse las lentes de contacto, y la composición no contiene cloruro de benzalconio.The present invention further relates to the use of an effective anti-allergic amount of a medication selected from the group consisting of olopatadine and emedastine and its pharmaceutically acceptable salts, in combination with a polymeric quaternary ammonium compound as a preservative, for the preparation of a topically administrable composition for treat or control eye allergies in patients who carry contact lenses and in which the composition can be applied without take off contact lenses, and the composition does not contain benzalkonium chloride

Descripción detallada de la invenciónDetailed description of the invention

La olopatadina es ácido de (Z)-11-(3-dimetilaminopropiliden)-6,11-dihidrodibenc[b,e]-oxepin-2-acético. La olopatadina puede hacerse usando los métodos descritos en la Patente de EE.UU. núm. 5.116.863. La concentración de olopatadina en las composiciones de la presente invención oscilarán de 0,0001 a 5% (peso/volumen), preferiblemente de 0,001 a 0,25% (peso/volumen), y lo más preferiblemente de 0,1 a 0,25% (peso/volumen), basado en el agua purificada esterilizada. El ingrediente de olopatadina puede estar presente en la forma de una sal farmacéuticamente aceptable. A menos que se indique otra cosa, la "olopatadina" como se usa aquí, se refiere tanto a la olopatadina como a sus sales farmacéuticamente aceptables. La forma más preferida de olopatadina es el hidrocloruro de olopatadina. La concentración más preferida de hidrocloruro de olopatadina es de 0,111 a 0,222% (peso/volumen), que es equivalente a 0,1 a 0,2% (peso/volumen) de olopatadina.Olopatadine is acid from (Z) -11- (3-dimethylaminopropylidene) -6,11-dihydrodibenc [b, e] -oxepin-2-acetic acid. Olopatadine can be made using the methods described in the U.S. Patent no. 5,116,863. Olopatadine concentration in the compositions of the present invention they will range from 0.0001 to 5% (weight / volume), preferably 0.001 to 0.25% (weight / volume), and most preferably from 0.1 to 0.25% (weight / volume), based on purified sterilized water. The ingredient of olopatadine may be present in the form of a pharmaceutically salt acceptable. Unless otherwise indicated, "olopatadine" as used herein, it refers to both olopatadine and its pharmaceutically acceptable salts. The most preferred form of olopatadine is olopatadine hydrochloride. The most concentration Preferred olopatadine hydrochloride is 0.111 to 0.222% (weight / volume), which is equivalent to 0.1 to 0.2% (weight / volume) of olopatadine

El nombre químico de la emedastina es 1-(2-etoxietil)-2-(4-metil-1-homopiper-azinil)-bencimidazol. El uso oftálmico de la emedastina se describe en la Patente de EE.UU. núm. 5.441.958. La emedastina puede hacerse usando los métodos descritos en la Patente de EE.UU. núm. 4.430.343. La concentración de emedastina en las composiciones de la presente invención oscilará de 0,0001 a 1% (peso/volumen), preferiblemente de 0,005 a 0,1% (peso/volumen), y lo más preferiblemente de 0,05% (peso/volumen). El ingrediente de emedastina puede estar presente en la forma de una sal farmacéuticamente aceptable. A menos que se indique otra cosa, la "emedastina" como se usa aquí se refiere tanto a la emedastina como a sus sales farmacéuticamente aceptables. La forma más preferida de la emedastina en el difumarato de emedastina. La concentración más preferida de difumarato de emedastina es 0,0884% (peso/volumen), que es equivalente a 0,05% (peso/volumen) de emedastina.The chemical name of emedastine is 1- (2-Ethoxyethyl) -2- (4-methyl-1-homopiper-azinyl) -benzimidazole. The ophthalmic use of emedastine is described in the USA no. 5,441,958. Emedastine can be done using the methods described in US Pat. no. 4,430,343. The Emedastine concentration in the compositions herein invention will range from 0.0001 to 1% (weight / volume), preferably from 0.005 to 0.1% (weight / volume), and most preferably 0.05% (weight / volume). Emedastine ingredient may be present. in the form of a pharmaceutically acceptable salt. Unless I know indicate otherwise, "emedastine" as used herein refers to both emedastine and its salts pharmaceutically acceptable. The most preferred form of emedastine in the Emedastine Dipumate. The most preferred concentration of Emedastine difumarate is 0.0884% (weight / volume), which is equivalent to 0.05% (weight / volume) of emedastine.

Además de la olopatadina o la emedastina, o una sal farmacéuticamente aceptable de las mismas, las composiciones de la presente invención contienen un compuesto polimérico de amonio cuaternario como un conservante. Los compuestos poliméricos de amonio cuaternario útiles en las composiciones de la presente invención son los que tienen un efecto antimicrobiano, y que son oftálmicamente aceptables. Los compuestos preferidos de este tipo se describen en las Patentes de EE.UU. núms. 3.931.319; 4.027.020; 4.407.791; 4.525.346; 4.836.986; 5.037.647 y 5.300.287; y el documento WO 91/09523 (Dziabo et al.). El compuesto polimérico de amonio más preferido es poliquaternium-1, conocido de otra forma como Polyquad® u Onamer M®, con un peso molecular medio numérico entre 2.000 a 30.000. Preferiblemente, el peso molecular medio numérico está entre 3.000 a 14.000.In addition to olopatadine or emedastine, or a pharmaceutically acceptable salt thereof, the compositions of the present invention contain a polymeric quaternary ammonium compound as a preservative. The polymeric quaternary ammonium compounds useful in the compositions of the present invention are those that have an antimicrobial effect, and that are ophthalmically acceptable. Preferred compounds of this type are described in US Pat. no. 3,931,319; 4,027,020; 4,407,791; 4,525,346; 4,836,986; 5,037,647 and 5,300,287; and WO 91/09523 (Dziabo et al .). The most preferred polymeric ammonium compound is polyquaternium-1, otherwise known as Polyquad® or Onamer M®, with a number average molecular weight between 2,000 to 30,000. Preferably, the number average molecular weight is between 3,000 to 14,000.

Los compuestos poliméricos de amonio cuaternario se usan generalmente en las composiciones de la presente invención en una cantidad de 0,00001 a 3% (peso/volumen), preferiblemente de 0,001 a 0,1% (peso/volumen). Lo más preferiblemente, las composiciones de la presente invención contienen de 0,001 a 0,05% (peso/volumen) de compuestos poliméricos de amonio cuaternario.The polymeric quaternary ammonium compounds they are generally used in the compositions of the present invention in an amount of 0.00001 to 3% (weight / volume), preferably of 0.001 to 0.1% (weight / volume). Most preferably, the Compositions of the present invention contain from 0.001 to 0.05% (weight / volume) of polymeric quaternary ammonium compounds.

Sería necesario o deseable añadir ácido bórico a las composiciones para alcanzar niveles deseados de eficacia de conservación. Véase la Patente de EE.UU. núm. 5.603.929. El ácido bórico adecuado para usar en las composiciones de la presente invención incluye no sólo ácido bórico, sino también sus sales de adición de ácido oftálmicamente aceptables, además de complejos borato-poliol del tipo descrito en la Patente de EE.UU. núm. 5.342.620 (Chowhan). Si está presente, la cantidad de ácido bórico oscilará generalmente de 0,3 a 5,0% (peso/volumen).It would be necessary or desirable to add boric acid to the compositions to achieve desired levels of efficacy of conservation. See US Pat. no. 5,603,929. Acid boric acid suitable for use in the compositions herein invention includes not only boric acid, but also its salts of addition of ophthalmically acceptable acid, in addition to complexes borate-polyol of the type described in the Patent of USA no. 5,342,620 (Chowhan). If present, the amount of boric acid will generally range from 0.3 to 5.0% (weight / volume).

Las composiciones de la presente invención deberían tener una tonicidad oftálmicamente aceptable, tal como 260-320 mOsm/kg, y un pH oftálmicamente aceptable, tal como pH 5-8, y preferiblemente pH 6,8-7,6. Las composiciones multi-dosis, administrables tópicamente, de la presente invención, comprenden opcionalmente otros excipientes, tales como agentes ajustadores de la tonicidad, agentes tamponantes, agentes quelantes, y agentes ajustadores de pH. Por ejemplo, cloruro sódico, mannitol, o similares, pueden usarse como el agente isotónico; hidrogenofosfato sódico, dihidrogenofosfato sódico, éster del ácido p-hidroxibenzóico, ácido bórico o similares como el agente tamponante; edetato sódico o similares como el agente quelante o estabilizador; e hidróxido sódico, ácido clorhídrico o similares como el agente ajustador de pH.The compositions of the present invention they should have an ophthalmically acceptable tonicity, such as 260-320 mOsm / kg, and an ophthalmically acceptable pH, such as pH 5-8, and preferably pH 6.8-7.6. The compositions multi-dose, topically administrable, of the present invention, optionally comprise other excipients, such as tonicity adjusting agents, agents buffers, chelating agents, and pH adjusting agents. By example, sodium chloride, mannitol, or the like, can be used as the isotonic agent; sodium hydrogen phosphate, dihydrogen phosphate sodium, p-hydroxybenzoic acid ester, acid boric or the like as the buffering agent; sodium edetate or similar as the chelating agent or stabilizer; and hydroxide sodium, hydrochloric acid or the like as the adjusting agent of pH

Las composiciones de la presente invención puede incluir además agentes modificadores de la viscosidad tales como: éteres celulósicos, tales como, hidroxipropilmetilcelulosa (HPMC), hidroxietilcelulosa (HEC), etilhidroxietilcelulosa, hidroxipropilcelulosa, metilcelulosa, y carboximetilcelulosa; carbómeros (por ejemplo, Carbopol®; poli(alcohol de vinilo); poli(pirrolidona de vinilo); alginatos; carrageenans; y gomas de guar, karaya, agarosa, algarroba y xantano.The compositions of the present invention may also include viscosity modifying agents such as: cellulosic ethers, such as, hydroxypropyl methylcellulose (HPMC), hydroxyethylcellulose (HEC), ethylhydroxyethylcellulose, hydroxypropyl cellulose, methyl cellulose, and carboxymethyl cellulose; carbomers (for example, Carbopol®; poly (vinyl alcohol); poly (vinyl pyrrolidone); alginates; carrageenans; and rubber of guar, karaya, agarose, carob and xanthan.

Los siguientes ejemplos se presentan para ilustrar diversos aspectos adicionales de la presente invención, pero no intentan limitar el alcance de la invención en ningún respecto.The following examples are presented for illustrate various additional aspects of the present invention, but they do not attempt to limit the scope of the invention in any respect.

Ejemplo 1Example 1

1one

Ejemplo 2Example 2

22

Claims (19)

1. Una composición anti-alérgica multi-dosis, administrable tópicamente, adecuada para usar por pacientes que llevan lentes de contacto, en la que la composición comprende una cantidad anti-alérgica eficaz de un medicamento seleccionado del grupo que consiste en olopatadina y emedastina y sus sales farmacéuticamente aceptables, y un compuesto polimérico de amonio cuaternario oftálmicamente aceptable como un conservante, con la condición de que la composición no contiene cloruro de benzalconio.1. An anti-allergic composition multi-dose, topically administrable, adequate for use by patients wearing contact lenses, in which the composition comprises an anti-allergic amount Effective of a drug selected from the group consisting of olopatadine and emedastine and their pharmaceutically acceptable salts, and an ophthalmically polymeric quaternary ammonium compound acceptable as a preservative, provided that the composition does not contain benzalkonium chloride. 2. La composición según la reivindicación 1, en la que el medicamento es olopatadina o una sal farmacéuticamente aceptable de la misma, y la cantidad anti-alérgica eficaz de olopatadina es de 0,0001 a 5% (peso/volumen).2. The composition according to claim 1, in which medicine is olopatadine or a pharmaceutically salt acceptable of it, and the anti-allergic amount Effective of olopatadine is 0.0001 to 5% (weight / volume). 3. La composición según la reivindicación 2, en la que la cantidad anti-alérgica eficaz de olopatadina es de 0,001 a 0,25% (peso/volumen).3. The composition according to claim 2, in which the effective anti-allergic amount of olopatadine is 0.001 to 0.25% (weight / volume). 4. La composición según la reivindicación 3, en la que el medicamento es hidrocloruro de olopatadina, y la cantidad anti-alérgica eficaz de olopatadina es de 0,1 a 0,25% (peso/volumen).4. The composition according to claim 3, in the medicine is olopatadine hydrochloride, and the amount Effective anti-allergic olopatadine is 0.1 to 0.25% (weight / volume). 5. La composición según la reivindicación 1, en la que el medicamento es emedastina o una sal farmacéuticamente aceptable de la misma, y la cantidad anti-alérgica eficaz de emedastina es de 0,0001 a 1% (peso/volumen).5. The composition according to claim 1, in which drug is emedastine or a pharmaceutically salt acceptable of it, and the anti-allergic amount Emedastine effective is 0.0001 to 1% (weight / volume). 6. La composición según la reivindicación 5, en la que la cantidad anti-alérgica eficaz de emedastina es de 0,005 a 0,1% (peso/volumen).6. The composition according to claim 5, in which the effective anti-allergic amount of Emedastine is 0.005 to 0.1% (weight / volume). 7. La composición según la reivindicación 5, en la que el medicamento es difumarato de emedastina, y la cantidad anti-alérgica eficaz de difumarato de emedastina es 0,0884% (peso/volumen).7. The composition according to claim 5, in which the medicine is emedastine diphemarate, and the amount Effective anti-allergic emedastine dipumate is 0.0884% (weight / volume). 8. La composición según una cualquiera de las reivindicaciones 1 a 7, en la que el compuesto polimérico de amonio cuaternario es poliquaternium-1.8. The composition according to any one of the claims 1 to 7, wherein the polymeric ammonium compound Quaternary is polyquaternium-1. 9. La composición según la reivindicación 8, en la que el compuesto polimérico de amonio cuaternario está presente en una cantidad de 0,00001 a 3% (peso/volumen).9. The composition according to claim 8, in which the quaternary ammonium polymer compound is present in an amount of 0.00001 to 3% (weight / volume). 10. La composición según la reivindicación 9, en la que el compuesto polimérico de amonio cuaternario está presente en una cantidad de 0,001 a 0,1% (peso/volumen).10. The composition according to claim 9, in which the quaternary ammonium polymer compound is present in an amount of 0.001 to 0.1% (weight / volume). 11. La composición según una cualquiera de las reivindicaciones 1 a 10, en la que la composición comprende además uno o más ingredientes seleccionados del grupo que consiste en agentes ajustadores de la tonicidad; agentes tamponantes; agentes quelantes; agentes ajustadores de pH; y agentes modificadores de la viscosidad.11. The composition according to any one of the claims 1 to 10, wherein the composition further comprises one or more ingredients selected from the group consisting of tonicity adjusting agents; buffering agents; agents chelators; pH adjusting agents; and agents modifying the viscosity. 12. El uso de una cantidad anti-alérgica eficaz de un medicamento seleccionado del grupo que consiste en olopatadina y emedastina, y sus sales farmacéuticamente aceptables, en combinación con un compuesto polimérico de amonio cuaternario como un conservante, para la preparación de una composición administrable tópicamente, para tratar o controlar las alergias oculares en pacientes que llevan lentes de contacto, en el que la composición puede aplicarse sin quitarse las lentes de contacto, y la composición no contiene cloruro de benzalconio.12. The use of a quantity effective anti-allergic of a selected medication from the group consisting of olopatadine and emedastine, and their salts pharmaceutically acceptable, in combination with a compound polymeric quaternary ammonium as a preservative, for the preparation of a topically administrable composition, for treat or control eye allergies in patients who carry contact lenses, in which the composition can be applied without take off contact lenses, and the composition does not contain benzalkonium chloride 13. El uso según la reivindicación 12, en el que el medicamento es olopatadina o una sal farmacéuticamente aceptable de la misma, y la cantidad anti-alérgica eficaz de olopatadina es de 0,0001 a 5% (peso/volumen).13. The use according to claim 12, wherein the medicine is olopatadine or a pharmaceutically acceptable salt of it, and the effective anti-allergic amount of olopatadine is 0.0001 to 5% (weight / volume). 14. El uso según la reivindicación 13, en el que el medicamento es hidrocloruro de olopatadina, y la cantidad anti-alérgica eficaz de olopatadina es de 0,1 a 0,25% (peso/volumen).14. The use according to claim 13, wherein the medicine is olopatadine hydrochloride, and the amount Effective anti-allergic olopatadine is 0.1 to 0.25% (weight / volume). 15. El uso según la reivindicación 12, en el que el medicamento es emedastina o una sal farmacéuticamente aceptable de la misma, y la cantidad anti-alérgica eficaz de emedastina es de 0,005 a 0,1% (peso/volumen).15. The use according to claim 12, wherein the medicine is emedastine or a pharmaceutically acceptable salt of it, and the effective anti-allergic amount of Emedastine is 0.005 to 0.1% (weight / volume). 16. El uso según la reivindicación 15, en el que el medicamento es difumarato de emedastina, y la cantidad anti-alérgica eficaz de difumarato de emedastina es 0,0884% (peso/volumen).16. The use according to claim 15, wherein the medicine is emedastine dipumarate, and the amount Effective anti-allergic emedastine dipumate is 0.0884% (weight / volume). 17. El uso según una cualquiera de las reivindicaciones 12 a 16, en el que el compuesto polimérico de amonio cuaternario es poliquaternium-1.17. Use according to any one of the claims 12 to 16, wherein the polymeric compound of Quaternary ammonium is polyquaternium-1. 18. El uso según la reivindicación 17, en el que el compuesto polimérico de amonio cuaternario está presente en una cantidad de 0,00001 a 3% (peso/volumen).18. The use according to claim 17, wherein the polymeric quaternary ammonium compound is present in a Amount from 0.00001 to 3% (weight / volume). 19. El uso según una cualquiera de las reivindicaciones 12 a 18, en el que la composición comprende además uno o más ingredientes seleccionados del grupo que consiste en agentes ajustadores de la tonicidad; agentes tamponantes; agentes quelantes; agentes ajustadores de pH; y agentes modificadores de la viscosidad.19. Use according to any one of the claims 12 to 18, wherein the composition further comprises one or more ingredients selected from the group consisting of tonicity adjusting agents; buffering agents; agents chelators; pH adjusting agents; and agents modifying the viscosity.
ES01906672T 2000-01-25 2001-01-24 ANTIALERGIC OPHTHALMIC COMPOSITIONS SUITABLE FOR USE WITH CONTACT LENSES. Expired - Lifetime ES2236180T3 (en)

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